Assay Detail
Functional
CHEMBL696210
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The compound was tested for the inhibition of all-trans retinoic acid (ATRA) catabolism using 7.27 pmol [11,12-3H]-ATRA as substrate in microsomal preparations of male hamster liver fortified with NADPH
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cricetulus griseus |
| Tissue | Liver |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Potent inhibition of retinoic acid metabolism enzyme(s) by novel azolyl retinoids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.90 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL57765 | — | — | 1 | 7.00 |
| CHEMBL431135 | — | — | 1 | 6.17 |
| CHEMBL417769 | — | — | 1 | 6.06 |
| CHEMBL53449 | — | — | 1 | 5.79 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 4.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL57765 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL431135 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL417769 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL53449 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 34000.0 | nM | 4.47 |